A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of wh...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2020-05, Vol.56 (41), p.5532-5535
Hauptverfasser: Kounde, Cyrille S, Shchepinova, Maria M, Saunders, Charlie N, Muelbaier, Marcel, Rackham, Mark D, Harling, John D, Tate, Edward W
Format: Artikel
Sprache:eng
Schlagworte:
HeLa Cells
Humans
Ligands
Light
Molecular Structure
Photodegradation
Proteins
Proteolysis
Ubiquitin-Protein Ligases - metabolism
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Beschreibung
Zusammenfassung:With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy. Caging of a widely used Von Hippel Lindau E3 ligase ligand for targeted protein degradation with PROTACs allows light-activated proteolysis.
ISSN:1359-7345
1364-548X
DOI:10.1039/d0cc00523a